Synthesis and antimicrobial activity of some novel 1,2-dihydro-[1,2,4]triazolo[1,5-]pyrimidines bearing amino acid moiety

• Published in: RSC advances Vol. 11; no. 5; pp. 295 - 2916
• Main Authors: Mohamed, Mounir A. A, Bekhit, Adnan A, Abd Allah, Omyma A, Kadry, Asmaa M, Ibrahim, Tamer M, Bekhit, Salma A, Amagase, Kikuko, El-Saghier, Ahmed M. M
• Format: Journal Article
• Language: English
• Published: England Royal Society of Chemistry 13-01-2021; The Royal Society of Chemistry
• Subjects: Antimicrobial agents; Bacteria; Chemical synthesis; Chemistry; Chloromycetin; Pyrimidines; Selectivity; Triazoles
• ISSN: 2046-2069; 2046-2069
• DOI: 10.1039/d0ra08189b

A new series of [1,2,4]-triazole bearing amino acid derivatives
2a-d
-
9a-d
were synthesized under green chemistry conditions
via
multicomponent reaction using lemon juice as an acidic catalyst. The obtained compounds were characterized by different spectral and elemental analyses. The obtained candidates showed promising antibacterial activity against some standard bacteria and multidrug resistant (MDR) clinical isolates. In contrast to the reference drugs cephalothin and chloramphenicol, the tested compounds showed substantial better MIC values towards the tested MDR strains. The most active compounds
3c
,
8a
and
9d
against MDR bacteria were tested for MBC and MIC index, the results indicted the bacteriostatic activity of these compounds. The most active compounds
2c
,
2d
,
3c
,
8a
,
8b
,
9a
,
9b
,
9c
and
9d
showed a high selectivity index towards antimicrobial activity against
K. pneumoniae
and
MRSA1
compared to mammalian cells, suggesting a good safety profile.
A new series of [1,2,4]-triazole bearing amino acid derivatives were synthesized under green chemistry conditions and evaluated for their antimicrobial activities.